结肠特异性给药系统卡培他滨片的处方、优化及评价

Hussain Mobarak, D. Biswajit, Chakraborty Jashabir
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引用次数: 4

摘要

目的:研究结肠癌特异性快速崩解卡培他滨片的研制与优化。方法:以交联棉糖钠(CCS)为超级崩解剂,采用直接加压法制备卡培他滨结肠靶向核心片,并采用不同比例的果胶加压包衣法制备核心片。采用浸渍包衣法,将ES100与邻苯二甲酸纤维素(CAP)按不同比例进行结肠靶向包衣。在不同pH值(1.2、6.8和7.4)下进行体外肿胀研究。使用Design Expert软件(v.10)优化最佳配方,并以时间间隔(2hr, 7hr和9hr)为可靠变量,确定药物在不同溶出介质(pH 1.2,6.8和7.4)中的体外累积释放百分比。结果:优化后的卡培他滨片在压缩前、压缩后的各项试验参数均达到满意的效果,且在30、60天的稳定性研究中具有显著的稳定性。结论:通过以上研究发现,缩短半衰期的抗癌药物卡培他滨的优化配方可以在果胶和乌木糖s100的帮助下,适当地靶向结肠区域。
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Formulation, Optimization and Evaluation of Capecitabine Tablet for Colon Specific Drug Delivery System
Aim: The present research is focused on development and optimization of colon specific, fast disintegrating Capecitabine tablet for the treatment of Colon cancer. Methods: Colon targeted core tablet of Capecitabine was prepared by using CCS (Croscarmellose sodium) as a super disintegrating agent by direct compression method and coating was done over the core tablets by using pectin in different ratios by compression coating method. The colon targeted coating was done on the compression coated tablets by using ES100 and CAP (Cellulose acetate phthalate) in different ratios by dip coating method. In vitro swelling studies were carried out at different pH (1.2, 6.8 and 7.4). The Design Expert software (v.10) was used to optimise the best formulation and an in vitro cumulative percentage of drug release in different dissolution media (pH 1.2, 6.8 and 7.4) with respect to the time interval (2hr, 7hr and 9hr) as dependable variable. Results: Optimized formulation of Capecitabine tablet shows satisfactory result with respect to all pre and post compression test parameters and it was significantly stable during stability studies conducted for 30and 60 days. Conclusion: From the above research it was found that, the optimised formulation of less half-life period anticancer drug Capecitabine can be properly targeted to colon area with the help of pectin and eudragit S 100.
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